This invention relates to the oral administration of a composition of matter having the therapeutic property of alleviating the craving for nicotine that accompanies the nicotine withdrawal syndrome.
Therapeutic efforts to break the tobacco smoking habit either through psychological approaches or through the use of various filters or cigarette substitutes have met with varying degrees of sucess.
It is generally recognized that bio-feedback from altered physical states can exert an influence on the psyche. The altered physical state induced by tobacco influences the psyche to an extent sufficient to account for a significant measure of its habit forming potential. This physiological component of the cigarette habit can be treated by oral therapy.
It is common knowledge that smokers who quit the habit tend to gain weight. Usually they crave sweets and in satisfying that craving they gain weight. Physicians cite cases of smokers who have broken the habit only to return to smoking owing to undesirable weight gain.
At the University of Wisconsin students were asked to place a thin wire through a small opening in a copper plate without touching the sides of the opening. An electric counter recorded the number of times contact was made with the sides of the opening. Smokers scored 60% poorer than nonsmokers. This strongly suggests that tremors were present in a greater degree in the smokers than in nonsmokers.
A successful oral therapeutic approach to tabacco withdrawal symptoms must therefore alleviate the two physical effects of the tobacco habit cited above, i.e., weight gain and tremors.
Tobacco smoke produces changes almost identical with that produced by adrenaline, including a rise in blood sugar. Nicotine, through its effect on the adrenals, increases the metabolic rate. Tobacco smoke also causes increases of oxygen consumption by an average of 30%. It is known that the potassium content of the blood rises and falls in parallel with the sugar content of the blood. This potassium and glucose tide accounts for some of the habit forming potential of nicotine addiction.
Some of the euphoria accompanying tobacco usage is due to the rise in both metabolic rate and blood sugar. Adrenaline secretion is increased by nicotine stimulation. Since adrenaline is a potent inhibitor of insulin, it not only provides glucose to the circulation, but also, because it decreases glucose uptake by peripheral tissues, glucose is preferentially preserved for utilization by the brain. This accounts for the improved capacity for mental concentration asserted by tobacco users.
Initially, nicotine stimulates the adrenal medulla and epinephrine is thereby discharged. This initial phase is transient and is followed by a paralysis of the secretory process. The degree of hypoglycemia which follows the primary rise in blood sugar may amount to a drop to 50-70 mgs/100 ml. The glycogen stores of the brain and nerves are very small. Hence a minute-to-minute supply of glucose is particularly important to the nervous system.
The dependence of various tissues upon circulating blood glucose varies widely. The central nervous system is perhaps most critically dependent, since glucose is the only nutrient that crosses the blood-brain barrier at a rate sufficient to sustain normal function. If the blood-glucose concentration falls abruptly, the earliest symptoms observed are referrable to the central nervous system.
The fall in blood sugar is accompanied by a fall in blood potassium. A low potassium blood level (hypokalemia) is associated with irritability, tremors, nervousness and electrocardiograph changes such as ST segment depression and T-wave inversion.
In tobacco withdrawal there are tremors, anxiety, nervousness, craving and irritability. EKGs taken on chronic smokers exhibit a decrease in amplitude or inversion of the T-wave.
I have discovered that the craving and habit forming aspect of tobacco withdrawal has a physiological component that is caused by the associated hypoglycemia and hypokalemia. It becomes apparent that the effects of nicotine stimulation produce an initial "lift" which is followed by a period of mild depression accompanied by bodily changes of the nature described above. Owing to the reciprocity existing between emotional experiences and physiological changes, the physiological changes noted above contribute, through bio-feedback, to the emotional dependence on the tobacco habit.
It is known that the elevation of the metabolic rate by as much as 25% can be achieved by the administration of caffeine. In addition, it is known that caffeine is also a powerful stimulant of the central nervous system. Its main action on the cortex is on psychic and sensory functions. It produces a clearer flow of thought, and motor activity is also improved.